In vitro and in vivo anti-angiogenic activities of Panduratin A.

<h4>Background</h4>Targeting angiogenesis has emerged as an attractive and promising strategy in anti-cancer therapeutic development. The present study investigates the anti-angiogenic potential of Panduratin A (PA), a natural chalcone isolated from Boesenbergia rotunda by using both in...

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Autores principales: Siew-Li Lai, Shiau-Chuen Cheah, Pooi-Fong Wong, Suzita Mohd Noor, Mohd Rais Mustafa
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Publicado: Public Library of Science (PLoS) 2012
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spelling oai:doaj.org-article:292ba60d41ed469db4d1ed0c6bd5e3242021-11-18T07:16:53ZIn vitro and in vivo anti-angiogenic activities of Panduratin A.1932-620310.1371/journal.pone.0038103https://doaj.org/article/292ba60d41ed469db4d1ed0c6bd5e3242012-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/22666456/pdf/?tool=EBIhttps://doaj.org/toc/1932-6203<h4>Background</h4>Targeting angiogenesis has emerged as an attractive and promising strategy in anti-cancer therapeutic development. The present study investigates the anti-angiogenic potential of Panduratin A (PA), a natural chalcone isolated from Boesenbergia rotunda by using both in vitro and in vivo assays.<h4>Methodology/principal findings</h4>PA exerted selective cytotoxicity on human umbilical vein endothelial cells (HUVECs) with IC(50) value of 6.91 ± 0.85 µM when compared to human normal fibroblast and normal liver epithelial cells. Assessment of the growth kinetics by cell impedance-based Real-Time Cell Analyzer showed that PA induced both cytotoxic and cytostatic effects on HUVECs, depending on the concentration used. Results also showed that PA suppressed VEGF-induced survival and proliferation of HUVECs. Furthermore, endothelial cell migration, invasion, and morphogenesis or tube formation demonstrated significant time- and dose-dependent inhibition by PA. PA also suppressed matrix metalloproteinase-2 (MMP-2) secretion and attenuated its activation to intermediate and active MMP-2. In addition, PA suppressed F-actin stress fiber formation to prevent migration of the endothelial cells. More importantly, anti-angiogenic potential of PA was also evidenced in two in vivo models. PA inhibited neo-vessels formation in murine Matrigel plugs, and angiogenesis in zebrafish embryos.<h4>Conclusions/significance</h4>Taken together, our study demonstrated the distinctive anti-angiogenic properties of PA, both in vitro and in vivo. This report thus reveals another biological activity of PA in addition to its reported anti-inflammatory and anti-cancer activities, suggestive of PA's potential for development as an anti-angiogenic agent for cancer therapy.Siew-Li LaiShiau-Chuen CheahPooi-Fong WongSuzita Mohd NoorMohd Rais MustafaPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 7, Iss 5, p e38103 (2012)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Siew-Li Lai
Shiau-Chuen Cheah
Pooi-Fong Wong
Suzita Mohd Noor
Mohd Rais Mustafa
In vitro and in vivo anti-angiogenic activities of Panduratin A.
description <h4>Background</h4>Targeting angiogenesis has emerged as an attractive and promising strategy in anti-cancer therapeutic development. The present study investigates the anti-angiogenic potential of Panduratin A (PA), a natural chalcone isolated from Boesenbergia rotunda by using both in vitro and in vivo assays.<h4>Methodology/principal findings</h4>PA exerted selective cytotoxicity on human umbilical vein endothelial cells (HUVECs) with IC(50) value of 6.91 ± 0.85 µM when compared to human normal fibroblast and normal liver epithelial cells. Assessment of the growth kinetics by cell impedance-based Real-Time Cell Analyzer showed that PA induced both cytotoxic and cytostatic effects on HUVECs, depending on the concentration used. Results also showed that PA suppressed VEGF-induced survival and proliferation of HUVECs. Furthermore, endothelial cell migration, invasion, and morphogenesis or tube formation demonstrated significant time- and dose-dependent inhibition by PA. PA also suppressed matrix metalloproteinase-2 (MMP-2) secretion and attenuated its activation to intermediate and active MMP-2. In addition, PA suppressed F-actin stress fiber formation to prevent migration of the endothelial cells. More importantly, anti-angiogenic potential of PA was also evidenced in two in vivo models. PA inhibited neo-vessels formation in murine Matrigel plugs, and angiogenesis in zebrafish embryos.<h4>Conclusions/significance</h4>Taken together, our study demonstrated the distinctive anti-angiogenic properties of PA, both in vitro and in vivo. This report thus reveals another biological activity of PA in addition to its reported anti-inflammatory and anti-cancer activities, suggestive of PA's potential for development as an anti-angiogenic agent for cancer therapy.
format article
author Siew-Li Lai
Shiau-Chuen Cheah
Pooi-Fong Wong
Suzita Mohd Noor
Mohd Rais Mustafa
author_facet Siew-Li Lai
Shiau-Chuen Cheah
Pooi-Fong Wong
Suzita Mohd Noor
Mohd Rais Mustafa
author_sort Siew-Li Lai
title In vitro and in vivo anti-angiogenic activities of Panduratin A.
title_short In vitro and in vivo anti-angiogenic activities of Panduratin A.
title_full In vitro and in vivo anti-angiogenic activities of Panduratin A.
title_fullStr In vitro and in vivo anti-angiogenic activities of Panduratin A.
title_full_unstemmed In vitro and in vivo anti-angiogenic activities of Panduratin A.
title_sort in vitro and in vivo anti-angiogenic activities of panduratin a.
publisher Public Library of Science (PLoS)
publishDate 2012
url https://doaj.org/article/292ba60d41ed469db4d1ed0c6bd5e324
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AT suzitamohdnoor invitroandinvivoantiangiogenicactivitiesofpanduratina
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